ORALLY ADMINISTERED IRINOTECAN HC1 IN PATIENTS W/ ADVANCED SOLID TUMORS

伊立替康(CPT-11)是喜树碱的半合成衍生物，通过抑制拓扑异构酶I发挥作用。我们的假设是口服盐酸伊立替康(CPT-11)是一种有效的抗肿瘤药物。我们正在进行口服盐酸伊立替康(CPT-11)对晚期实体肿瘤患者的I期试验。该试验的目标是：1)测定CPT-11每三周连续五天口服一次时的MTD和DLT；2)确定按此时间表口服CPT-11时的安全性；3)研究CPT-11及其代谢物SN-38和SN-38葡萄糖醛酸苷(SN-38G)的单剂量和多剂量药代动力学；4)检测任何抗肿瘤活性的证据。目前的试验处于应计阶段的早期阶段，共有6名患者参加了两种不同剂量水平的试验。在第一周期的第一天和第五天进行药代动力学采样。该研究药物由Pharmacia和Upjohn提供。关于未来研究的计划目前还在等待中。

Irinotecan (CPT-11) is a semisynthetic derivative of camptothecin which acts by inhibiting topoisomerase I. It is our hypothesis that orally administered irinotecan HC1 (CPT-11) is a potent and effective antitumor agent. We are undertaking a phase I trial of oral irinotecan HC1 (CPT-11) in patients with advanced solid tumors. The objectives of the trial are: 1) to determine the MTD and the DLT of CPT-11 when administered orally once per day for five consecutive days every three weeks, 2) to define the safety profile of CPT-11 when administered orally on this schedule, 3) to characterize the single- and multiple-dose pharmacokinetics of CPT-11 and its metabolites, SN-38 and SN-38 glucuronide (SN-38G), and 4) to detect any evidence of antitumor activity. The current trial is very early in the accrual stage with a total of six patients enrolled at two different dose levels. Pharmacokinetic sampling is being performed on days one and five of cycle one. The study drug is being supplied by Pharmacia and Upjohn. Plans for future studies are pending at this time.